999-01-9Relevant academic research and scientific papers
ENPP1 INHIBITORS AND THEIR USE FOR THE TREATMENT OF CANCER
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Paragraph 00338; 00339, (2019/04/09)
Compounds, compositions and methods are provided for the inhibition of ENPP1. Aspects of the subject methods include contacting a sample with a ENPP1 inhibitor to inhibit cGAMP hydrolysis activity of ENPP1. In some cases, the ENPP1 inhibitor is cell impermeable. Also provided are compositions and methods for treating cancer. Aspects of the methods include administering to a subject a therapeutically effective amount of a ENPP1 inhibitor to treat the subject for cancer. In certain cases, the cancer is a solid tumor cancer. Also provided are methods of administering radiation therapy to a subject either before or after administering an ENPP1 inhibitor. The radiation therapy can be administered at a dosage and/or frequency effective to reduce radiation damage to the subject. In certain cases, the method is performed in combination with a chemotherapeutic agent, or a checkpoint inhibitor, or both.
Synthetic method of methyl phosphite and glufosinate-ammonium
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Paragraph 0029, (2016/11/07)
The invention discloses a synthetic method of methyl phosphite and glufosinate-ammonium. The method comprises the steps: with phosphorus pentasulfide as a starting material, then carrying out vulcanization reaction, chlorination reaction, water washing and distillation purification, then carrying out catalytic hydrogenation to obtain chloride phosphite (III), and next carrying out Grignard reaction to obtain methyl phosphite (IV), wherein R is C1-C4 alkyl. The method comprises the steps: with phosphorus pentasulfide as the starting material, then carrying out vulcanization reaction, chlorination reaction, water washing and distillation purification, then carrying out catalytic hydrogenation to obtain chloride phosphite, next carrying out Grignard reaction to synthesize methyl phosphite (IV), and thus obtaining the final product glufosinate-ammonium through a Strecker route of the prior art. The synthetic yield is increased, methyl phosphorus dichloride and other unstable corrosive intermediates cannot be produced, the discharge of three-waste substances is reduced, and environment-friendly costs and pressure are reduced.
Radical addition reactions of phosphorus hydrides: Tuning the reactivity of phosphorus hydrides, the use of microwaves and horner-wadsworth-emmons-type reactions
Jessop, Christopher M.,Parsons, Andrew F.,Routledge, Anne,Irvine, Derek J.
, p. 1547 - 1554 (2007/10/03)
The reactivity of phosphorus hydrides in radical addition reactions are compared, and the substituents on phosphorus are shown to affect the efficiency of the reactions. The change in reactivity is attributed to the different bond dissociation energies of the P-H bonds, which have been calculated. Phosphorus hydrides with particularly weak P-H bonds are shown to undergo radical additions by microwave irradiation, in the absence of conventional initiators. These radical addition reactions produce phosphonothioates, phosphinothioates and phosphane sulfides, which react in HWE-type reactions, to afford substituted alkenes. copy; Wiley-VCH Verlag GmbH & Co. KGaA, 2006.
Phosphonodifluoromethyl and phosphonothiodifluoromethyl radicals. Generation and addition onto alkenes and alkynes
Pignard, Sebastien,Lopin, Chrystel,Gouhier, Geraldine,Piettre, Serge R.
, p. 31 - 37 (2007/10/03)
Selanylated difluoromethylphosphonates and difluoromethylphosphonothioates are good precursors to phosphonodifluoromethyl and phosphonothiodifluoromethyl radicals, respectively. When generated in the presence of alkenes and a hydrogen donor, the corresponding α,α-difluorinated alkylphosphonates or alkylphosphonothioates are produced in fair to good yields. The use of alkynes results in the formation of α,α-difluorinated allyl derivatives in useful yields. The presence of the sulfur atom in phosphonothiodifluoromethyl radicals usually translates into higher isolated yields.
The preparation and properties of some α-acyloxy- and α-carbamoyloxy-phosphonothionates
Hudson, Harry R.,Jaszay, Zsuzsa M.,Pianka, Max
, p. 1571 - 1582 (2007/10/03)
New α-acyloxy and α-carbamoyloxy derivatives of dimethyl 2,2,2-trichloroethyl-phosphonothionate have been prepared, characterized, and screened for activity against free-living soil nematodes. Several of the more easily hydrolysable esters, and also the N-methylcarbamoyl derivative, were as active as the parent pesticide, dimethyl α-hydroxy2,2,2-trichloroethylphosphonothionate, after an induction period during which the active species is assumed to be released in vivo. It is concluded that the 2,2,2-trichloroethyl group is essential for activity in compounds of these types and that the presence of the N-methylcarbamoyl group does not in itself confer activity.
Reactions of Three-Coordinate Phosphorus(V) Compounds S=P(R)=S with Diethyl Phosphonate
Popova,Ishmaeva,Patsanovskii,Efremov,Rizvanov
, p. 240 - 241 (2007/10/03)
Dithioxophosphorane S=P(2,4,6-t-Bu3C6H2)=S reacts with diethyl phosphonate under mild conditions with thionation of the phosphonate (an O,S exchange reaction) to form as major products O,O-diethyl phosphonothioate and the cyclic trimer [-(Ar)P(O)-]3.
Reactions of P_Cl compounds in presence of SMI2
Sasaki, Mitsuru,Collin, Jacqueline,Kagan, Henri B.
, p. 2493 - 2496 (2007/10/02)
Conversion of P-Cl to P-H and P-C bonds are induced by SmI2 in mild conditions. Especially phosphines oxides and sulfides are obtained in good yields.
A facile conversion of dialkyl phosphonates to dialkyl phosphorodithioates
Wada,Hata
, p. 7461 - 7462 (2007/10/02)
Dialkyl phosphonates were converted into the corresponding phosphorodithioates in three steps by one-pot procedure. The reaction was applied to the synthesis of nucleoside phosphorodithioate derivatives.
